• Title/Summary/Keyword: Antinociceptive activity

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Anti-nociceptive and Anti-inflammatory Properties of Ilex latifolia and its Active Component, 3,5-Di-caffeoyl Quinic Acid Methyl Ester

  • Kim, Joo Youn;Lee, Hong Kyu;Seong, Yeon Hee
    • Natural Product Sciences
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    • v.25 no.1
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    • pp.64-71
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    • 2019
  • The present study was conducted to investigate anti-nociceptive and anti-inflammatory effects of the leaves of Ilex latifolia Thunb (I. latifolia) in in vivo and in vitro. Writhing responses induced by acetic acid and formalin- and thermal stimuli (tail flick and hot plate tests)-induced pain responses for nociception were evaluated in mice. I. latifolia (50 - 200 mg/kg, p.o.) and ibuprofen (100 mg/kg, p.o.), a positive non-steroidal anti-inflammatory drug (NSAID), inhibited the acetic acid-induced writhing response and the second phase response (peripheral inflammatory response) in the formalin test, but did not protect against thermal nociception and the first phase response (central response) in the formalin test. These results show that I. latifolia has a significant anti-nociceptive effect that appears to be peripheral, but not central. Additionally, I. latifolia (50 and $100{\mu}g/mL$) and 3,5-di-caffeoyl quinic acid methyl ester ($5{\mu}M$) isolated from I. latifolia as an active compound significantly inhibited LPS-induced NO production and mRNA expression of the pro-inflammatory mediators, iNOS and COX-2, and the pro-inflammatory cytokines, IL-6 and $IL-1{\beta}$, in RAW 264.7 macrophages. These results suggest that I. latifolia can produce antinociceptive effects peripherally, but not centrally, via anti-inflammatory activity and supports a possible use of I. latifolia to treat pain and inflammation.

Methanol extracts of Asarum sieboldii Miq. induces apoptosis via the caspase pathway in human FaDu hypopharynx squamous carcinoma cells

  • Lee, Seul Ah;Park, Bo-Ram;Kim, Chun Sung
    • International Journal of Oral Biology
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    • v.46 no.2
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    • pp.85-93
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    • 2021
  • Asarum sieboldii Miq. (Aristolochiaceae) is a perennial herbaceous plant and has been used as traditional medicine for treating diseases, cold, fever, phlegm, allergies, chronic gastritis, and acute toothaches. Also, it has various biological activities, such as antiallergic, antiinflammatory, antinociceptive, and antifungal. However, the anticancer effect of A. sieboldii have been rarely reported, except anticancer effect on lung cancer cell (A549) of water extracts of A. sieboldii. This study investigated the anticancer activity of methanol extracts of A. sieboldii (MeAS) and the underlying mechanism in human FaDu hypopharyngeal squamous carcinoma cells. MeAS inhibited FaDu cells grown dose-dependently without affecting normal cells (L929), as determined by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide and live and dead assay. In addition, concentration of MeAS without cytotoxicity (0.05 and 0.1 mg/mL) inhibited migration and colony formation. Moreover, MeAS treatment significantly induced apoptosis through the proteolytic cleavage of caspase-3, -7, -9, poly (ADP-ribose) polymerase, and downregulation of Bcl-2 and upregulation of Bax in FaDu cells, as determined by fluorescence-activated cell sorting analysis, 4'6-diamidino-2-phenylindole stain, and western blotting. Altogether, these results suggest that MeAS exhibits strong anticancer effects by suppressing the growth of oral cancer cells and the migration and colony formation via caspase- and mitochondrial-dependent apoptotic pathways in human FaDu hypopharyngeal squamous carcinoma cells. Therefore, MeAS can serve as a natural chemotherapeutic for human oral cancer.

The Analgesic Effect and the Mechanism of Electroacupuncture on Thermal Hyperalgesia in the Rat Model of Collagenase-induced Arthritis: Mediation by Adrenergic Receptors (Collagenase-induced Arthritis Rat Model에서 Thermal Hyperalgesia에 대한 전침(電鍼)의 진통효과(鎭痛效果) 및 기전연구: Adrenergic Mechanism에 대(對)한 연구(硏究))

  • Seo, Byung-Kwan;Park, Dong-Suk;Baek, Yong-Hyeon
    • Journal of Acupuncture Research
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    • v.28 no.2
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    • pp.57-67
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    • 2011
  • 목적 : Collagenase-induced osteoarthritis(OA) 동물 모델에서 전침의 adrenergic mechanism을 연구하고자 한다. 방법 : Collagenase-induced arthritis(CIA)를 유발하기 위하여 5주령의 male Sprague-Dawley rat의 뒷다리 좌측 무릎 관절에 0.05ml의 4mg/ml collagenase solution을 intra-articular 주입하고, 다시 4일 후에 같은 부위에 같은 농도의 collagenase solution을 intra-articular boosting injection 시행한 뒤, gross, histopathological features 및 biomarker activity 변화를 관찰하였다. 예비실험을 통하여 CIA rat model에서 진통효과를 발휘하는 것으로 확인한, 족삼리(足三里) ($ST_{36}$)에 대한 저빈도 train pulse EA stimulation (2Hz, 0.07 mA, 0.3ms)을 침치료 방법으로 적용하였다. 전침의 진통기전을 확인하기 위하여, ${\alpha}1$-adrenergic antagonist (prazosin, 1 mg/kg, i.p.), ${\alpha}2$-adrenergic receptor antagonist (yohimbine, 2mg/kg, i.p.), ${\alpha}1$-adrenergic receptor agonist(phenylephrine, 2mg/kg, i.p.), ${\alpha}2$-adrenergic receptor agonist(clonidine, $40{\mu}g$/kg, i.p.)을 전침시행 20분 전에 복강 내로 전처치하였다. Tail flick unit(Ugo Basile Model 7360)을 이용하여 열자극에 대한 통증역치를 측정하였다. 결과 : 퇴행성관절염 징후(gross, histopathological features)와 통증역치의 변화가 최대값을 나타내는 CIA 유발 4주차에 저빈도 전침자극(train pulse, 2Hz, 0.07mA, 0.3ms)을 족삼리($ST_{36}$)에 적용하였으며, 족삼리 전침의 진통효과는 ${\alpha}2$-adrenergic receptor antagonist(yohimbine, 2mg/kg, i.p.)전처치에 의해 억제되었으나, ${\alpha}1$-adrenergic antagonist(prazosin, 1 mg/kg, i.p.)전처치에는 억제되지 않았다. 또 ${\alpha}2$-adrenergic receptor agonist(clonidine, $40{\mu}g$/kg, i.p.)의 전처치를 통하여 유의한 synergistic analgesic effect가 관찰되었으나, ${\alpha}1$-adrenergic receptor agonist(phenylephrine, 2mg/kg, i.p.)의 전처치는 전침의 진통효과에 synergistic effect를 미치지 않는 것으로 나타났다. 결론 : 저빈도 족삼리 전침은 CIA로 유발된 염증성 통증에 대하여 진통효과를 발휘하며, 이는 ${\alpha}2$-adrenergic receptor에 의하여 매개되는 것으로 보이며 ${\alpha}1$-adrenergic receptor는 영향을 미치지 않는 것으로 사료된다.

Effects of Ethanol Extract from Lathyrus palustris on Anti-inflammation Response of RAW 264.7 Cell (RAW 264.7 대식세포 염증반응에 대한 털연리초 에탄올 추출물의 항염증 효과)

  • Nam, Jung Hwan
    • Korean Journal of Plant Resources
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    • v.33 no.4
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    • pp.287-292
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    • 2020
  • Lathyrus palustris often used as a treatment for inflammation of the kidneys in Korean traditional medication. Generally, drugs for arthritis have anti-inflammatory and antinociceptive properties. However, the validity of the anti-inflammatory effect has not been scientifically investigated so far. Therefore, the purpose of the research was to investigate the latent anti-inflammatory ability of L. palustris using the ethanol extract. To evaluate the anti-inflammatory activities, we examined the inflammatory arbitrators such as a nitric oxide (NO) and prostaglandin E2 (PGE2) on RAW 264.7 cells. Our results indicated that ethanol extract significantly inhibited the lipopolysaccharide E (LPS) derived PGE2 production in RAW 264.7 cell. The inhibitory activity of ethanol extract for PGE2 tests with inhibition ratio showed in 40 ㎍/mL. Overall, PGE2 tests had a higher inhibitory effect on inflammation than NO tests. This result anticipated that the ethanol extract from L. palustris is a good candidate for developing the origin of anti-inflammatory agents.

Inhibitory Effects of Extracts from Arabis glabra on Lipopolysaccharide Induced Nitric Oxide and Prostaglandin E2 Production in RAW264.7 Macrophages (RAW264.7 대식세포에서 장대나물 추출물의 Nitric oxide 및 Prostaglandin E2생성 저해효과)

  • Nam, Jung-Hwan;Seo, Jong-Taek;Kim, Yul-Ho;Kim, Ki-Deog;Yoo, Dong-Lim;Lee, Jong-Nam;Hong, Su-Young;Kim, Su-Jeong;Sohn, Hwang-Bae;Kim, Hyun-Sam;Kim, Bo-Sung;Shin, Ji-Sun;Lee, Kyung-Tea;Park, Hee-Jhun
    • Korean Journal of Plant Resources
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    • v.28 no.5
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    • pp.568-573
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    • 2015
  • Arabis glabra is a localized common rhizomatous flowering plant, This plant is often used in Korean traditional systems of medicine as a remedy for blood cleaning, detoxification, abscess, gastrospasm, arthritis, contraction and diarrhea. Generally drugs that are used for arthritis have antinociceptive and anti-inflammatory properties. However, validity of the anti-inflammatory activity has not been scientifically investigated so far. Therefore, the aim of this study was to investigate the anti-inflammatory potential of A. glabra using the ethanolic extract and its sub-fractions. To evaluate the anti-inflammatory effects, we examined the inflammatory mediators such as nitric oxide (NO) and prostaglandin E2 (PGE2) on RAW 264.7macrophages. Our results indicated that hexane and chloroform fraction significantly inhibited the LPS-induced NO and PGE2 production in the cells. The hexane fraction inhibitory activity for NO tests with IC50 values showed in 21.0 ㎍/㎖. The chloroform fraction inhibitory activity for PGE2 tests with IC50 values showed in 18.0 ㎍/㎖. These efficacy are expected to be able to present the potential for the development of health functional food for the prevention inflammatory diseases because it has sufficient preventive medical possibilities. Further, it is determined that it is necessary to further study the mechanism of cytokine and protein expression associated with inflammation.

In vitro anti-inflammatory activity of extracts from Potentilla supina in murine macrophage RAW 264.7 cells (개소시랑개비 추출물의 RAW264.7대식세포에서 in vitro 항염효과)

  • Nam, Jung-Hwan;Kim, Hyun-Sam;Kim, Byoumg-Jin;Yu, Hong-Seob;Chang, Dong-Chil;Jin, Yong-Ik;Yoo, Dong-Lim;Choi, Jong-Keun;Park, Hee-Jhun;Lee, Seung-Bin;Lee, Kyung-Tea;Park, Soo-Jin
    • Journal of Plant Biotechnology
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    • v.44 no.1
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    • pp.76-81
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    • 2017
  • Potentilla supina (Rosaceae) has traditionally been used to treat disorders of hemostasis, dysentery, malaria, bloody discharge and arthritis, and it has antinociceptive and anti-inflammatory properties. However, validity of the anti-inflammatory activity has not been scientifically investigated so far. Therefore, the aim of this study was to investigate the anti-inflammatory potential of P. supina using the ethanolic extract of P. supina and its sub-fractions. To evaluate the anti-inflammatory effects of P. supina, we examined the inflammatory mediators such as nitric oxide (NO), inducible nitric oxide synthase (iNOS) and prostaglandin $E_2$ ($PGE_2$) in RAW 264.7 cells. Our results indicated that ethyl acetate fraction significantly inhibited LPS-induced NO, iNOS and $PGE_2$ production in RAW 264.7 cells. This result showed that ethyl acetate fraction of P. supina is expected to be a good candidate for development into a source of anti-inflammatory agents.

Inhibitory effects of extracts from Smilacina japonica on lipopolysaccharide induced nitric oxide and prostaglandin E2 production in RAW264.7 macrophages (RAW264.7 대식세포에서 풀솜대 추출물의 nitric oxide 및 prostaglandin E2생성 저해효과)

  • Nam, Jung-Hwan;Seo, Jong-Taek;Kim, Yul-Ho;Kim, Ki-Deog;Yoo, Dong-Lim;Lee, Jong-Nam;Hong, Su-Young;Kim, Su-Jeong;Sohn, Hwang-Bae;Kim, Hyun-Sam;Kim, Bo-Sung;Lee, Kyung-Tea;Park, Hee-Jhun
    • Journal of Plant Biotechnology
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    • v.41 no.4
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    • pp.201-205
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    • 2014
  • Smilacina japonica is a localized common rhizomatous flowering plant, This plant is often used in Korean traditional systems of medicine as a remedy for migrain, diplegia, physical impurity, blood circulation, abscess and contusion. Generally drugs that are used for arthritis have antinociceptive and anti-inflammatory properties. However, validity of the anti-inflammatory activity has not been scientifically investigated so far. Therefore, the aim of this study was to investigate the anti-inflammatory potential of S. japonica using the ethanolic extract and its subfractions. To evaluate the anti-inflammatory effects, we examined the inflammatory mediators such as nitric oxide (NO) and prostaglandin $E_2$ ($PGE_2$) on RAW 264.7 macrophages. Our results indicated that hexane fraction significantly inhibited the LPS induced NO and $PGE_2$ production in the cells. The hexane fractions inhibitory activity for NO tests with $IC_{50}$ values showed in $53.3{\mu}g/ml$ and $PGE_2$ tests with $IC_{50}$ values showed at $32.5{\mu}g/ml$. Theseis result suggest a potential role of hexane fraction from S. japonica as source of anti-inflammatory agent.

Antinociceptive Effect of Testosterone in Androgenized Female Mice (남성화된 암컷 생쥐에서 Testosterone이 통각예민도에 미치는 영향)

  • Chon, Myong-Ho;Kim, Myung-Jung;Park, Je-Min;Yang, Gu-Beum;Lee, Kook-Hee;Jang, Sae-Heon;Kang, Cheol-Joong
    • Korean Journal of Psychosomatic Medicine
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    • v.8 no.1
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    • pp.65-71
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    • 2000
  • Objects : Aimed to test the hypothesis that neonatal testosterone exposure in female mice influences the development of testosterone-related pain inhibitory system and that testosterone administered in adulthood decreases the pain sensitivity. Methods : Thirty androgenized(testosterone propionate $100{\mu}g$ ip within 24 hrs after birth) adult female and twenty five control(normal saline $100{\mu}g$ ip within 24 hrs after birth) adult female mice were injected with testosterone propionate 1mg/kg/day for 3 consecutive days from 84th experimental days. Nociceptive sensitivity was measured before and after treatment of testosterone by tail flick latency on 84th and 86th experimental days. Results : 1) On the 84th experimental day, basal nociceptive sensitivity was significantly higher in the androgenized group($2.7{\pm}0.4$ sec) as compared to the control group($3.3{\pm}1.1$ sec). 2) Testosterone treatment on the 84th experimental day significantly lowered nociceptive sensitivity in both androgenized($5.2{\pm}0.9$ sec) and control groups($4.6{\pm}1.8$ sec). However the effect was significantly greater in the androgenized group. 3) Nociceptive sensitivity on 86th experimental day before administration of testosterone was significantly lower in the androgenized group($4.8{\pm}1.9$ sec) as compared to the control group($3.9{\pm}1.2$ sec). 4) Testosterone treatment on the 86th experimental day significantly lowered the nociceptive sensitivity in both groups, but the androgenized group($5.9{\pm}0.9$ sec) showed significantly lower post-treatment nociceptive sensitivity as compared to the control group($4.9{\pm}1.5$ sec). 5) Nociceptive sensitivity was decreased significantly after injection of testosterone once a day for two consecutive days in the androgenized group(${\Delta}2.1{\pm}1.0$ sec), but not in the control group(${\Delta}0.5{\pm}1.3$ sec). Conclusions : There may be a testosterone-related pain inhibitory system, the development of which is enhanced by exposure to testosterone in the neonatal period, and the activity of which is also mediated by testosterone in the later life.

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